In recent years, deep mycoses caused by opportunistic fungal infection have been increasing with the frequent use of steroids, carcinostatic agents, and immunosuppressants as well as with the prevalence of acquired immunodeficiency syndrome (AIDS).
Conventional antifungals involve various clinical problems and are not necessarily deemed to be satisfactory drugs. For example, amphotericin B, though exhibiting extremely potent antifungal activities, also has serious side effects, such as hyperthermia and renal insufficiency, which have limited usefulness of the drug. 5-Fluorocytosine is apt to develop resistant fungi. Ketoconazole induces hepatotoxicity following maintained administration of large doses and, in addition, oral preparations but not intravenous injections are available. On the other hand, fluconazole has been frequently used clinically because of its relatively low toxicity and availability in both oral preparations and intravenous injections. However, it has a low inhibitory activity against aspergillosis, and the development of resistance has recently given rise to a problem. Further, itraconazole, of the same triazole type, is only available in oral preparations and cannot be administered to those patients who cannot receive a treatment by mouth. It is also deemed unsatisfactory in terms of potency and pharmacokinetics.
Deep mycoses are, for the most part, candidosis, cryptococcosis, and aspergillosis, and how to treat these infectious diseases, especially aspergillosis has been a clinically important subject.
EP 0421210A2 and JP-A-58-189173 (the term "JP-A" as herein means an "unexamined published Japanese patent application" disclose 1-aryl-2-(1H-1,2,4-triazol-1-yl)-ethanol derivatives but gives no mention of the specific compound of the present invention.